Levobunolol (Betagan) Eye Drops - Uses, Dose, MOA, Brands, Side effects

Levobunolol is a medication primarily used to treat high pressure inside the eye due to glaucoma or other eye diseases (ocular hypertension). It belongs to a class of drugs called beta-blockers, which work by decreasing the production of fluid inside the eye, thereby lowering intraocular pressure.

Reducing intraocular pressure is crucial in managing conditions like glaucoma because elevated pressure can damage the optic nerve, leading to vision loss or blindness if left untreated.

Levobunolol (Betagan) is used to reduce intraocular pressure by increasing the outflow of aqueous humor and decreasing its production.

Levobunolol Uses:

  • Raised intraocular pressure:
    • used to treat individuals with ocular hypertension or persistent open-angle glaucoma who have increased intraocular pressure

Levobunolol (Betagan) Dose in Adults:

Levobunolol (Betagan) Dose in the therapy of Elevated intraocular pressure:

  • When treating high pressure inside the eye, you usually put 1 or 2 drops of levobunolol into the affected eye once a day.
  • If your glaucoma is severe or not under control, your doctor may tell you to use 1 drop twice a day instead.
  • But using more than 1 drop twice a day usually doesn't work any better.

·


 

Use in Children:

Not indicated.


Pregnancy Risk Category: C

  • Using levobunolol in your eyes can cause similar side effects as taking beta-blockers by mouth.
  • If you're pregnant and need eye drops for glaucoma, doctors recommend using the smallest effective dose along with closing the tear ducts to reduce any risk to the baby.

Use during breastfeeding:

  • We're not sure if levobunolol passes into breast milk, but other beta-blockers taken by mouth or as eye drops have been found in breast milk.
  • If you're breastfeeding and need to use levobunolol, doctors suggest using the smallest effective dose and closing the tear ducts to reduce any risk to your baby.
  • The manufacturer advises caution when giving levobunolol to breastfeeding mothers.

Dose in Kidney Disease:

  • The manufacturer's instructions don't mention any specific changes in dosage for people with kidney problems.
  • If you have kidney issues and need to use levobunolol, it's essential to follow your doctor's advice carefully.
  • They'll monitor your condition and adjust your treatment as needed to ensure your safety and effectiveness of the medication.

Dose in Liver disease:

  • The manufacturer's instructions don't include any specific changes in dosage for individuals with liver problems.
  • If you have liver issues and need to use levobunolol, it's crucial to follow your doctor's guidance closely.
  • They will monitor your condition and adjust your treatment as necessary to ensure your safety and the effectiveness of the medication.

Common Side Effects of Levobunolol (Betagan):

  • Ophthalmic:
    • Stinging of eyes
    • Burning sensation of eyes

Less Common Side Effects of Levobunolol (Betagan):

  • Ophthalmic:
    • Ocular Allergy
    • Visual Disturbance
    • Blepharoconjunctivitis
    • Diplopia
    • Blepharoptosis
    • Decreased Corneal Sensitivity
    • Iridocyclitis
    • Keratitis
  • Neuromuscular & Skeletal:
    • Weakness
  • Cardiovascular:
    • Cardiac Failure
    • Cerebral Ischemia
    • Bradycardia
    • Cardiac Arrhythmia
    • Cerebrovascular Accident
    • Hypotension
    • Palpitations
    • Chest Pain
    • Heart Block
    • Syncope
  • Hypersensitivity:
    • Hypersensitivity Reaction
  • Central Nervous System:
    • Headache
    • Lethargy
    • Dizziness
    • Exacerbation Of Myasthenia Gravis
    • Ataxia (Transient)
    • Confusion
    • Depression
    • Foreign Body Sensation Of Eye
    • Paresthesia
  • Endocrine & Metabolic:
    • Hypoglycemia (Masked)
  • Dermatologic:
    • Skin Rash
    • Stevens-Johnson Syndrome
    • Alopecia
    • Pruritus
    • Urticaria
  • Gastrointestinal:
    • Diarrhea
    • Nausea
  • Genitourinary:
    • Impotence
  • Respiratory:
    • Dyspnea
    • Nasal Congestion
    • Bronchospasm
    • Respiratory Failure

Contraindications to Levobunolol (Betagan):

  • Levobunolol shouldn't be used if you're allergic to it or any of the ingredients in the medication, have a history of bronchial asthma or severe chronic obstructive pulmonary disease (COPD), experience very slow heart rate (sinus bradycardia), have certain heart rhythm disorders (second- or third-degree atrioventricular block), have heart failure, or are in cardiogenic shock.
  • While there isn't extensive evidence on cross-reactivity with other beta-adrenergic blocking agents for the eyes, due to similarities in their chemical structure and how they work, there's a possibility of allergic reactions.

Warnings and Precautions

Anaphylactic reactions

  • If you've had severe allergic reactions before, be careful when using levobunolol, especially if you've reacted to different allergens in the past.
  • Also, if you're taking beta-blockers like levobunolol, you might become more sensitive to allergens over time.
  • It's important to know that if you have an allergic reaction while on beta-blockers, treatments like epinephrine might not work as well or could cause unwanted effects.

Choroidal detachment:

  • Using beta-blockers like levobunolol or other medications that reduce fluid in the eye can sometimes lead to choroidal detachment, especially after certain eye surgeries like filtration procedures.
  • It's essential to be aware of this risk if you're undergoing such procedures and to discuss it thoroughly with your eye doctor.

Cerebrovascular disease

  • If you have cerebrovascular disease, be careful when using levobunolol, as it may affect blood flow to the brain.
  • If you start experiencing signs or symptoms of reduced blood flow to your brain after starting this treatment, talk to your doctor.
  • They can consider other options or adjust your treatment to ensure your safety and well-being.

Diabetes:

  • If you have diabetes, be cautious when using levobunolol, as it can affect your blood sugar levels.
  • Levobunolol may make episodes of low blood sugar (hypoglycemia) worse or hide the signs and symptoms of low blood sugar.
  • It's important to monitor your blood sugar levels regularly and discuss any concerns with your doctor.
  • They can help you manage your diabetes effectively while using this medication.

Heart failure:

  • If you have heart failure, be cautious when using levobunolol, especially if your condition is stable.
  • Monitor for any signs of your heart condition getting worse while using this medication.
  • Levobunolol may potentially worsen heart failure, especially if you didn't have heart failure before.
  • If you notice any signs or symptoms of heart failure, like shortness of breath or swelling, stop using levobunolol and contact your doctor immediately.
  • Levobunolol should not be used if you already have overt heart failure.
  • According to the American Heart Association (AHA), levobunolol is considered a medication that can significantly worsen underlying heart muscle dysfunction.

Myasthenia gravis:

  • If you have myasthenia gravis, be cautious when using levobunolol, as it may potentially worsen your condition or other symptoms associated with myasthenia gravis, such as double vision, drooping eyelids, or generalized weakness.
  • It's important to discuss your medical history, including any existing conditions like myasthenia gravis, with your doctor before starting levobunolol or any other medications.
  • They can help you weigh the benefits and risks and provide appropriate monitoring to ensure your safety while using this medication.

Respiratory disease

  • If you have peripheral vascular disease or Raynaud disease, be cautious when using levobunolol, as it may trigger or worsen symptoms of reduced blood flow in your arteries.
  • Levobunolol can potentially exacerbate symptoms of arterial insufficiency, such as coldness or numbness in the extremities.
  • It's important to use this medication with care and monitor for any signs of worsening arterial obstruction.
  • If you experience any new or worsening symptoms, particularly related to blood circulation, inform your doctor promptly.
  • They can assess your condition and adjust your treatment plan as needed to ensure your safety and well-being.

Raynaud and peripheral vascular disease:

  • If you have respiratory diseases like asthma or chronic obstructive pulmonary disease (COPD), it's typically not recommended to use beta-blockers like levobunolol.
  • However, if your doctor decides that it's necessary to use levobunolol, it should be done cautiously with close monitoring.
  • Serious respiratory reactions, including fatal bronchospasm, have been reported with the use of levobunolol in patients with asthma.
  • Levobunolol is contraindicated in individuals with bronchial asthma or a history of it, as well as in those with severe COPD.

Thyroid disease:

  • If you have thyroid disease, be aware that levobunolol may hide signs of an overactive thyroid gland, such as fast heartbeat.
  • If you suspect you have an overactive thyroid, your doctor will need to carefully manage and monitor your condition while you're using levobunolol.
  • Suddenly stopping levobunolol could make symptoms of an overactive thyroid worse or even lead to a dangerous condition called thyroid storm.

Levobunolol: Drug Interaction

Risk Factor C (Monitor therapy)

Bradycardia-Causing Agents

may intensify other bradycardia-causing agents' bradycardic effects.

Bupivacaine

Beta-blockers may raise the serum level of buprenorphine.

Cholinergic Agonists

Beta-Blockers may make Cholinergic Agonists' harmful or toxic effects worse. The possibilities for bronchoconstriction and aberrant cardiac conduction are of special concern.

EPINEPHrine (Nasal)

 The hypertensive impact of EPINEPHRINE may be enhanced by beta-blockers like Nonselective (Nasal).

EPINEPHrine (Oral Inhalation)

 The hypertensive impact of EPINEPHRINE may be enhanced by beta-blockers like Nonselective (Oral Inhalation).

Epinephrine (Racemic)

 Epinephrine's hypertensive action may be enhanced by beta-blockers like Nonselective (Racemic).

EPINEPHrine (Systemic)

 The hypertensive impact of EPINEPHRINE may be enhanced by beta-blockers like Nonselective (Systemic).

Ivabradine

 Bradycardia-Causing Agents may intensify Ivabradine's bradycardic impact.

Lacosamide

Bradycardia-Causing Substances may intensify Lacosamide's AV-blocking effects.

Lidocaine (Systemic)

Beta-blockers could boost the level of lidocaine in the blood (Systemic).

Lidocaine (Topical)

Beta-blockers could boost the level of lidocaine in the blood (Topical).

Mepivacaine

Mepivacaine's serum levels may rise after using beta-blockers.

Methacholine

Beta-Blockers could make methacholine's harmful or toxic effects worse.

Methoxyflurane

may strengthen beta-blockers' hypotensive effects.

Midodrine

Bradycardia-Causing Agents' bradycardic impact could be enhanced.

NIFEdipine

may strengthen beta-blockers' hypotensive effects. The detrimental inotropic impact of beta-blockers may be amplified by NIFEdipine.

Opioids (Anilidopiperidine

might make beta-blockers' bradycardic impact stronger. Beta-Blockers may have a greater hypotensive impact when combined with opioids (anilidopiperidine).

Regorafenib

might make beta-blockers' bradycardic impact stronger.

Reserpine

may strengthen beta-blockers' hypotensive effects.

Ruxolitinib

May enhance the bradycardic effect of Bradycardia-Causing Agents. Management: Ruxolitinib Canadian product labeling recommends avoiding use with bradycardia-causing agents to the extent possible.

Terlipressin

May enhance the bradycardic effect of Bradycardia-Causing Agents.

Theophylline Derivatives

Theophylline derivatives may not have the same bronchodilatory effects as beta-blockers as Nonselective.

Tofacitinib

Bradycardia-Causing Agents' bradycardic impact could be enhanced.

Risk Factor D (Consider therapy modification)

Ceritinib

Bradycardia-Causing Agents may enhance the bradycardic effect of Ceritinib. Management: If this combination cannot be avoided, monitor patients for evidence of symptomatic bradycardia, and closely monitor blood pressure and heart rate during therapy. Exceptions are discussed in separate monographs.

Dronedarone

May enhance the bradycardic effect of Beta-Blockers. Dronedarone may increase the serum concentration of Beta-Blockers. This likely applies only to those agents that are metabolized by CYP2D6. Management: Use lower initial beta-blocker doses; adequate tolerance of the combination, based on ECG findings, should be confirmed prior to any increase in betablocker dose.

Ergot Derivatives

Beta-Blockers may enhance the vasoconstricting effect of Ergot Derivatives. Exceptions: Nicergoline.

Fingolimod

Beta-Blockers may enhance the bradycardic effect of Fingolimod. Management: Avoid the concomitant use of fingolimod and beta-blockers if possible. If coadministration is necessary, patients should have overnight continuous ECG monitoring conducted after the first dose of fingolimod. Monitor patients for bradycardia.

Grass Pollen Allergen Extract (5 Grass Extract)

Beta-Blockers may enhance the adverse/toxic effect of Grass Pollen Allergen Extract (5 Grass Extract). More specifically, Beta-Blockers may inhibit the ability to effectively treat severe allergic reactions to Grass Pollen Allergen Extract (5 Grass Extract) with epinephrine. Some other effects of epinephrine may be unaffected or even enhanced (e.g., vasoconstriction) during treatment with Beta-Blockers.

Siponimod

Bradycardia-Causing Agents may enhance the bradycardic effect of Siponimod. Management: Avoid the coadministration of siponimod with drugs that may cause bradycardia.

Risk Factor X (Avoid combination)

Beta2-Agonists

Beta-Blockers (Nonselective) may diminish the bronchodilatory effect of Beta2Agonists.

Fexinidazole [INT]

Bradycardia-Causing Agents may enhance the arrhythmogenic effect of Fexinidazole [INT].

Floctafenine

May enhance the adverse/toxic effect of Beta-Blockers.

Rivastigmine

May improve the bradycardic effect of Beta-Blockers.

Monitoring parameters:

Intraocular Pressure:

  • Levobunolol is used to lower pressure inside the eye.
  • It's important to monitor this pressure regularly, especially if you have glaucoma or other eye conditions.

Heart Rate:

  • Levobunolol can affect your heart rate.
  • Your doctor may check your heart rate to make sure it stays within a safe range while using this medication.

Funduscopic Exam:

  • This is an eye exam that checks the back of your eye, including the retina.
  • Your doctor may perform this exam to monitor for any changes in your eye health while using levobunolol.

Visual Field Testing:

  • This test checks your peripheral vision.
  • Your doctor may use this test to see if levobunolol is effectively managing your condition and if there are any changes in your vision over time.

How to administer Levobunolol (Betagan)?

For Topical Ophthalmic Use Only:

  • Levobunolol is meant to be used only in the eyes.
  • It should not be taken by mouth or used on the skin.

Hand Hygiene:

  • Wash your hands before and after using levobunolol.
  • This helps prevent contamination and reduces the risk of spreading infections.

Contact Lens Use:

  • If you wear contact lenses, remove them before using levobunolol.
  • Wait at least 15 minutes before putting your lenses back in after using the medication.

Avoid Touching Tip:

  • Do not let the tip of the applicator touch your eye or any other surfaces.
  • This helps prevent contamination and keeps the medication sterile.

Avoid Using Multiple Beta-Blockers:

  • Do not use more than one beta-adrenergic blocking eye medication at the same time.
  • Using multiple medications of this type simultaneously can increase the risk of side effects and complications.

Mechanism of action of Levobunolol (Betagan):

  • Levobunolol blocks both beta- and beta-adrenergic receptors in the eye.
  • By doing this, it helps to lower the pressure inside the eye by either reducing the production of aqueous humor (the fluid in the eye) or possibly increasing its drainage out of the eye.
  • This mechanism of action helps to manage conditions like glaucoma by reducing the pressure that can damage the optic nerve and impair vision.

Onset of Action: Within 1 Hour

  • Levobunolol typically starts working within one hour after administration.
  • This means that it begins to reduce intraocular pressure relatively quickly after being applied to the eye.

Peak Effect: 2 to 6 Hours

  • The maximum effect of levobunolol is usually reached between 2 to 6 hours after administration.
  • During this time frame, the medication is most effective at lowering intraocular pressure.

Duration: Up to 24 Hours

  • Levobunolol can have a lasting effect, with its effects lasting for up to 24 hours.
  • This means that a single dose of levobunolol can provide consistent pressure-lowering effects throughout the day, reducing the need for frequent dosing.

International Brand Names of Levobunolol:

  • Betagan
  • APO-Levobunolol HCl
  • PMS-Levobunolol
  • RATIO-Levobunolol
  • SANDOZ Levobunolol
  • B-Tablock
  • Betagan
  • Betagen
  • Bunolgan
  • Evobun
  • Glubanol
  • Levosan
  • Levunolol
  • Mascglucom
  • Ocupress
  • Orbunol
  • Vistagan

Levobunolol Brand Names in Pakistan:

Levobunolol HCl Eye Drops 0.5 %w/v in Pakistan

Betagan

Barrett Hodgson Pakistan (Pvt) Ltd.

Levolol

Global Pharmaceuticals

Levoptic

Vega Pharmaceuticals Ltd.

Levosan

Sante (Pvt) Limited

Ocugan

Farmigea Pak (Pvt) Ltd.

Ophth-Levo

Ophth-Pharma (Pvt) Ltd.

Orbunol

Zafa Pharmaceutical Laboratories (Pvt) Ltd.

Vistagan

P.D.H. Pharmaceuticals (Pvt) Ltd.

Voben

Kobec Pharmacals